Lewis Roshan J, Mohr John F
Department of Internal Medicine, Division of Infectious Diseases and The Center for Emerging and Re-emerging Pathogens, The University of Texas Health Science Center at Houston, Houston, TX, USA.
Drug Saf. 2008;31(4):283-92. doi: 10.2165/00002018-200831040-00002.
The fluoroquinolones are an extremely popular class of antibacterials, owing to their broad spectrum of activity and the convenience of their intravenous and oral dosage formulations. Overall, the currently available fluoroquinolones have a good safety profile; however, certain fluoroquinolones within the class have been associated with severe and life-threatening adverse drug reactions. Dysglycaemic episodes (hyperglycaemia and hypoglycaemia) have been observed in patients taking multiple antibacterials, including the fluoroquinolones. Although gatifloxacin has been associated with dysglycaemias more frequently than other fluoroquinolones, dysglycaemic events have been reported with some of the other currently available fluoroquinolones as well. Hypoglycaemia appears to be related to insulin release and is an early-onset event. However, hyperglycaemia tends to present several days into therapy and the exact mechanism by which it is caused is still unclear. Recent studies point towards the important role of the adenosine triphosphate (ATP)-sensitive K+ channels in the pancreatic beta cell and the importance of anti-insulin hormones. Several retrospective studies have elucidated risk factors associated with fluoroquinolone exposure and subsequent dysglycaemic events. These studies suggest that dysglycaemia is a dose-related adverse effect involving the fluoroquinolone class; however, some drugs within the class appear to have a greater association. This may be related to the affinity of fluoroquinolones to the ATP-sensitive K+ channel or higher concentrations of drugs achieved in certain patients who are already at risk for hyperglycaemia and hypoglycaemia. Understanding these risk factors will allow the fluoroquinolones to be utilized in a way that minimizes the probability of associated dysglycaemic events.
氟喹诺酮类是一类极其常用的抗菌药物，这归因于它们广泛的抗菌活性以及静脉和口服剂型的便利性。总体而言，目前可用的氟喹诺酮类药物安全性良好；然而，该类别中的某些氟喹诺酮类药物与严重且危及生命的药物不良反应相关。在服用包括氟喹诺酮类在内的多种抗菌药物的患者中，已观察到血糖异常事件（高血糖和低血糖）。尽管加替沙星比其他氟喹诺酮类药物更常与血糖异常相关，但其他一些目前可用的氟喹诺酮类药物也报告了血糖异常事件。低血糖似乎与胰岛素释放有关，是一种早期发生的事件。然而，高血糖往往在治疗几天后出现，其确切病因仍不清楚。最近的研究指出了三磷酸腺苷（ATP）敏感性钾通道在胰腺β细胞中的重要作用以及抗胰岛素激素的重要性。几项回顾性研究阐明了与氟喹诺酮类药物暴露及随后血糖异常事件相关的危险因素。这些研究表明，血糖异常是涉及氟喹诺酮类药物的剂量相关不良反应；然而，该类别中的某些药物似乎关联更大。这可能与氟喹诺酮类药物对ATP敏感性钾通道的亲和力有关，或者与某些已经有高血糖和低血糖风险的患者体内达到的更高药物浓度有关。了解这些危险因素将有助于以降低相关血糖异常事件发生概率的方式使用氟喹诺酮类药物。
